规格 | 价格 | 库存 | 数量 |
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体外研究 (In Vitro) |
沙鼠中的脑酶被 30 µmol/kg 口服剂量(12.64 µg/kg Ro 61-8048,化合物 16)抑制。这种抑制作用在 2 小时后达到峰值(约 85% 抑制)并持续长达 8 小时[1]。 Ro 61-8048 (0.1-100 μM) 显着抑制 QUIN 的形成,表明犬尿氨酸羟化酶活性是 QUIN 体外新合成所必需的[3]。
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体内研究 (In Vivo) |
在 dtsz 仓鼠中,Ro 61-8048(50、100 和 150 mg/kg ip)可显着减轻肌张力障碍的严重程度,且不会产生明显的中枢副作用[2]。在突变仓鼠的纹状体、小脑和脑干中,Ro 61-8048(100 mg/kg ip)会导致内源性广谱谷氨酸受体拮抗剂犬尿氨酸增加两到三倍[2]。
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动物实验 |
Animal/Disease Models: Male and female dtsz mutant Syrian golden hamsters[2].
Doses: 50, 100 and 150 mg /kg. Route of Administration: IP, one dose. Experimental Results: Dramatically decreased the individual maximum severity of dystonia reached at the end of the observation period of 3 h at doses of 50, 100 and 150 mg/kg ip. 100 and 150 mg/kg Dramatically diminished the severity, indicating a fast onset of action. A delayed onset of dystonic attacks was observed after treatment with 150 mg/kg but not after administration of 50 and 100 mg/kg. At lower doses of 10 and 25 mg/kg, the compound failed to exert any antidystonic effects. Caused a moderate sedation and hypolocomotion 5 to 70 min after administration of 100 and 150 mg/kg, while no central adverse effects were observable at a dose of 50 mg/kg or lower doses. |
参考文献 |
[1]. S Röver, et al. Synthesis and biochemical evaluation of N-(4-phenylthiazol-2-yl)benzenesulfonamides as high-affinity inhibitors of kynurenine 3-hydroxylase. J Med Chem. 1997 Dec 19;40(26):4378-85.
[2]. Melanie Hamann, et al. Effects of the kynurenine 3-hydroxylase inhibitor Ro 61-8048 after intrastriatal injections on the severity of dystonia in the dt sz mutant. Eur J Pharmacol. 2008 May 31;586(1-3):156-9. [3]. AlbertoChiarugi, et al. Quinolinic acid formation in immune-activated mice: studies with (m-nitrobenzoyl)-alanine (mNBA) and 3,4-dimethoxy-[-N-4-(-3-nitrophenyl) thiazol-2yl]-benzenesulfonamide (Ro 61-8048), two potent and selective inhibitors of kynureni |
分子式 |
C17H15N3O6S2
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分子量 |
421.45
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CAS号 |
199666-03-0
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相关CAS号 |
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SMILES |
O=S(C1=CC=C(OC)C(OC)=C1)(NC2=NC(C3=CC=CC([N+]([O-])=O)=C3)=CS2)=O
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别名 |
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外) |
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溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.93 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (5.93 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 20 mg/mL (47.46 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 2.3728 mL | 11.8638 mL | 23.7276 mL | |
5 mM | 0.4746 mL | 2.3728 mL | 4.7455 mL | |
10 mM | 0.2373 mL | 1.1864 mL | 2.3728 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。